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CAS No. :
MCE 国际站:SEL120-34A monohydrochloride
产品活性:SEL120-34A monohydrochloride 是一种选择性的,ATP-竞争性的 CDK8 抑制剂,对 CDK8/CycC 和 CDK19/CycC 复合物的 IC50 值分别为 4.4 nM 和 10.4 nM,对 CDK8 的 Kd 值为 3 nM。SEL120-34A monohydrochloride 对 CDK9 的作用很弱,计算的 IC50 值为 1070 nM,而对 CDK1、2、4、6、5、7 等无作用。SEL120-34A monohydrochloride 能够抑制 STAT1 S727 和 STAT5 S726 的磷酸化。具有抗肿瘤活性。
研究领域:Cell Cycle/DNA Damage
作用靶点:CDK
In Vitro: SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50s of 4.4 nM and 10.4 nM, respectively, with a Kd of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC50=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7.
SEL120-34A (1.6 nM-5 μM) inhibits the growth of STAT5 S726 positive KG-1 AML cells, but is not cytotoxic to S726 negative MOLM13 AML cells.
SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726, decreases IRF9 and STAT1 mRNA expression and mitogen-induced IER expression.
In Vivo: SEL120-34A monohydrochloride (30, 60 mg/kg, p.o. once every day) inhibits growth of AML tumors in a dose-dependent manner in SCID mice after treatment for 17 days.
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